Acaluxen Capsule
Acalabrutinib
100 mg
Everest Pharmaceuticals Ltd.
| Pack size | 30's pack |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 1,000.00 AED |
Indications
Acaluxen Capsule is used for:
Mantle Cell Lymphoma
Adult Dose
Mantle Cell Lymphoma
Indicated for mantle cell lymphoma (MCL) in patients who have received ?1 prior therapy
100 mg PO every twelve hours
Continue until disease progression or unacceptable toxicity
Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
Indicated for treatment of chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)
Monotherapy
100 mg PO every twelve hours
Continue until disease progression or unacceptable toxicity
Combination with obinutuzumab
Indicated for patients with previously untreated CLL or SLL
Start acalabrutinib at Cycle 1 (each cycle is 28 days)
Start obinutuzumab at Cycle 2 for a total of 6 cycles
Refer to obinutuzumab for infusion rates
Cycle 1
Days 1-28: Acalabrutinib 100 mg PO q12hr
Cycle 2
Days 1-28: Acalabrutinib 100 mg PO q12hr
Day 1: Obinutuzumab 100 mg IV infusion
Day 2: Obinutuzumab 900 mg IV infusion
Days 8 and 15: Obinutuzumab 1000 mg IV infusion
Cycles 3-7
Day 1-28: Acalabrutinib 100 mg PO q12hr
Day 1: Obinutuzumab 1000 mg IV infusion
Cycle 8 and subsequent cycles
Day 1-28: Acalabrutinib 100 mg PO q12hr
Continue until disease progression or unacceptable toxicity
Child Dose
Renal Dose
Renal impairment
Mild-to-moderate (eGFR >30 mL/min/1.73m²): No clinically relevant pharmacokinetics (PK) difference observed
Severe (eGFR <30 mL/min/1.73m²) or patients on dialysis: Acalabrutinib PK has not been evaluated
Administration
Take with or without food
Contra Indications
Precautions
Serious hemorrhagic events, including fatal events, reported; the mechanism for the bleeding events is not well understood; acalabrutinib may further increase hemorrhage risk in patients receiving antiplatelet or anticoagulant therapies, and patients should be monitored for signs of bleeding; consider the benefit-risk of withholding acalabrutinib for 3-7 days presurgery and postsurgery depending on the type of surgery and the risk of bleeding
Serious infections (bacterial, viral, or fungal), including fatal events and opportunistic infections, reported; monitor for infection and consider prophylaxis in patients who are at increased risk for opportunistic infections
Cytopenias reported, including neutropenia, anemia, and thrombocytopenia; assess complete blood cell counts monthly during treatment
Second primary malignancies, including nonskin carcinomas, have occurred in patients with hematologic malignancies treated with acalabrutinib; the most frequent was skin cancer; advise patients regarding need for protection from sun exposure
Atrial fibrillation and flutter occurred (rare) during clinical trials; monitor patients and manage as appropriate
Monitoring Parameter
Monitor complete blood cell counts monthly during treatment
Monitor for symptoms of arrhythmia (eg, palpitations, dizziness, syncope, dyspnea)
Evaluate bilirubin and transaminases at baseline and throughout treatment; for patients who develop abnormal liver tests, monitor more frequently for liver test abnormalities and clinical signs and symptoms of hepatic toxicity.
Pregnancy-Lactation
Pregnancy
Based on findings in animals, may cause fetal harm when administered to pregnant women
There are no available data in pregnant women to inform the drug-associated risk
Pregnancy testing is recommended for females of reproductive potential before initiating therapy
Animal data
In animal reproduction studies, administration of acalabrutinib to pregnant rabbits during organogenesis resulted in reduced fetal growth; rabbit maternal exposures (AUC) were ~4 times that of humans given a dose of 100 mg BID
Advise pregnant women of the potential risk to a fetus
Contraception
Embryofetal harm and dystocia may occur when administered to pregnant women
Females of reproductive potential: Use effective contraception during treatment and for at least 1 week following the last dose; if used during pregnancy, or if the patient becomes pregnant while taking drug, inform patient of the potential hazard to a fetus
Lactation
No data are available regarding the presence of acalabrutinib or its active metabolite in human milk, its effects on the breastfed child, or on milk production
Acalabrutinib and its active metabolite were present in the milk of lactating rats
Owing to the potential for adverse reactions in a breastfed child, advise lactating women not to breastfeed while taking acalabrutinib and for at least 2 weeks after the final dose
Interactions
Coadministration with CYP3A inhibitors or inducers
Acalabrutinib is predominantly metabolized by CYP3A enzymes
CYP3A inhibitors are expected to increase acalabrutinib systemic exposure
CYP3A inducers are expected to decrease acalabrutinib systemic exposure
Coadministration with gastric acid-reducing agents
Coadministration with PPIs, H2-antagonists, or antacids may decrease acalabrutinib plasma concentrations
Contraindicated (0)
Serious - Use Alternative (59)
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Adverse Effects
Side effects of Acalabrutinib :
>10%
All grades
Decreased hemoglobin (46%)
Decreased platelets (44%)
Headache (39%)
Decreased neutrophils (36%)
Diarrhea (31%)
Fatigue (28%)
Myalgia (21%)
Bruising (21%)
Nausea (19%)
Rash (18%)
Abdominal pain (15%)
Constipation (15%)
Vomiting (13%)
Grade >3
Decreased neutrophils (15%)
Decreased platelets (12%)
1-10%
Increased creatinine, 1.5-3X ULN (4.8%)
All grades
Hemorrhage/hematoma (8%)
Epistaxis (6%)
Grade >3
Decreased hemoglobin (10%)
Diarrhea (3.2%)
Abdominal pain (1.6%)
Headache (1.6%)
Vomiting (1.6%)
Mechanism of Action
Bruton tyrosine kinase (BTK) inhibitor; acalabrutinib and its active metabolite, ACP-5862, form a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity
BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways; in B cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion
Note
Acaluxen 100 mg Capsule manufactured by Everest Pharmaceuticals Ltd.. Its generic name is Acalabrutinib. Acaluxen is availble in Bangladesh.
Farmaco BD drug index information on Acaluxen Capsule is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.